L-Methylfolate 7.5mg Tablets
It is used to aid diet needs.
Drug Class
Nutritional Supplement; Antianemic; Adjunctive therapy for depression/neuropathy
Pharmacologic Class
Folate derivative; B vitamin
Pregnancy Category
Category A
FDA Approved
Jan 1970
DEA Schedule
Not Controlled
Overview
What is this medicine?
L-methylfolate is the active form of a B vitamin called folate. It's essential for many body functions, including making important chemicals in your brain that affect mood, supporting nerve health, and helping produce red blood cells. It's especially helpful for people whose bodies have difficulty converting regular folic acid into its active form.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. It's essential to continue taking this medication as directed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store this medication at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore drug take-back programs in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food. It's essential to continue taking this medication as directed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store this medication at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medications, do not flush them down the toilet or pour them down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method. You may also want to explore drug take-back programs in your area.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Maintain a balanced diet rich in fruits, vegetables, and whole grains.
- Continue with other prescribed medications and therapies as directed by your healthcare provider.
- Report any new or worsening symptoms to your doctor.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
7.5 mg once daily
Dose Range:
7.5 - 15 mg
Condition-Specific Dosing:
Major Depressive Disorder (adjunctive):
7.5 mg to 15 mg once daily
Diabetic Peripheral Neuropathy:
7.5 mg to 15 mg once daily
Hyperhomocysteinemia:
7.5 mg to 15 mg once daily
Pediatric Dosing
Neonatal:
Not established for specific drug indications; general folate supplementation based on age/needs
Infant:
Not established for specific drug indications; general folate supplementation based on age/needs
Child:
Not established for specific drug indications; general folate supplementation based on age/needs
Adolescent:
Not established for specific drug indications; general folate supplementation based on age/needs
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Dialysis:
No adjustment needed; L-methylfolate is water-soluble and generally safe
Hepatic Impairment:
Mild:
No adjustment needed
Moderate:
No adjustment needed
Severe:
No adjustment needed
Pharmacology
Mechanism of Action
L-methylfolate is the primary active form of folate and the only form that can cross the blood-brain barrier. It is a cofactor in the synthesis of monoamines (serotonin, dopamine, norepinephrine) and is essential for DNA synthesis, repair, and methylation processes. It plays a critical role in the metabolism of homocysteine to methionine. In individuals with MTHFR polymorphisms, L-methylfolate bypasses the enzymatic step that converts inactive folic acid to active L-methylfolate, ensuring adequate folate levels for various metabolic functions.
Pharmacokinetics
Absorption:
Bioavailability:
High (>90%)
Tmax:
1-3 hours
FoodEffect:
Minimal
Distribution:
Vd:
Not available (widely distributed)
ProteinBinding:
Low
CnssPenetration:
Yes
Elimination:
HalfLife:
~3 hours (plasma), tissue stores longer
Clearance:
Not precisely quantified for L-methylfolate as a drug
ExcretionRoute:
Primarily renal, some biliary
Unchanged:
<5%
Pharmacodynamics
OnsetOfAction:
Weeks to months for full clinical effect (e.g., mood improvement), as it involves repletion of folate stores and downstream effects.
PeakEffect:
Varies by indication and individual folate status
DurationOfAction:
Sustained as long as supplementation continues and tissue stores are maintained.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
- Signs of an allergic reaction, such as rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you have side effects that bother you or do not go away, contact your doctor for advice.
Reporting Side Effects
This list does not include all possible side effects. If you have questions or concerns about side effects, discuss them with your doctor. For medical advice about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
- Signs of an allergic reaction, such as rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, trouble breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Other Possible Side Effects
Like all medications, this drug can cause side effects. However, many people do not experience any side effects or only have mild ones. If you have side effects that bother you or do not go away, contact your doctor for advice.
Reporting Side Effects
This list does not include all possible side effects. If you have questions or concerns about side effects, discuss them with your doctor. For medical advice about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Generally very well-tolerated with few side effects.
- Rarely, mild gastrointestinal upset (nausea, bloating) or sleep disturbances (insomnia or vivid dreams) may occur, especially at higher doses.
- If you experience any unusual or severe symptoms, contact your healthcare provider.
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions between this medication and other substances.
* Any existing health problems, as they may affect the safety and efficacy of this medication.
To ensure your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. It is vital to verify that it is safe to take this medication with all your other medications and health conditions. Your doctor and pharmacist will work together to assess potential interactions and determine the best course of treatment for you.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
All medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial to avoid potential interactions between this medication and other substances.
* Any existing health problems, as they may affect the safety and efficacy of this medication.
To ensure your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. It is vital to verify that it is safe to take this medication with all your other medications and health conditions. Your doctor and pharmacist will work together to assess potential interactions and determine the best course of treatment for you.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. If you have any concerns or questions, be sure to discuss them with your doctor.
If you are allergic to tartrazine, also known as FD&C Yellow No. 5, consult your doctor before taking this medication, as some products may contain this ingredient.
When taking cholestyramine or colestipol, it is crucial to consult with your pharmacist to determine the best way to take these medications in conjunction with this drug to ensure safe and effective use.
If you are pregnant, planning to become pregnant, or are breastfeeding, it is vital to discuss the potential benefits and risks of this medication with your doctor. This will help you make an informed decision about your treatment and the well-being of your baby.
If you are allergic to tartrazine, also known as FD&C Yellow No. 5, consult your doctor before taking this medication, as some products may contain this ingredient.
When taking cholestyramine or colestipol, it is crucial to consult with your pharmacist to determine the best way to take these medications in conjunction with this drug to ensure safe and effective use.
If you are pregnant, planning to become pregnant, or are breastfeeding, it is vital to discuss the potential benefits and risks of this medication with your doctor. This will help you make an informed decision about your treatment and the well-being of your baby.
Overdose Information
Overdose Symptoms:
- L-methylfolate has very low toxicity, and serious overdose symptoms are unlikely.
- Possible mild gastrointestinal upset (nausea, diarrhea).
What to Do:
Discontinue use and contact a healthcare professional or poison control center (1-800-222-1222) if you suspect an overdose, though severe effects are not expected.
Drug Interactions
Major Interactions
- Methotrexate (may reduce efficacy of methotrexate)
- Pyrimethamine (may reduce efficacy of pyrimethamine)
- Anticonvulsants (e.g., phenytoin, phenobarbital, primidone - L-methylfolate may reduce their levels or efficacy, and these drugs can also lower folate levels)
Moderate Interactions
- Sulfasalazine (can interfere with folate absorption/metabolism)
- Trimethoprim (can interfere with folate metabolism)
- Cholestyramine (may impair folate absorption)
Monitoring
Baseline Monitoring
Serum/RBC Folate levels
Rationale: To assess baseline folate status, especially if deficiency is suspected or for specific indications.
Timing: Prior to initiation
Homocysteine levels
Rationale: If indicated for conditions like hyperhomocysteinemia or cardiovascular risk assessment.
Timing: Prior to initiation
Clinical symptoms (e.g., mood, neuropathy)
Rationale: To establish baseline severity for conditions being treated.
Timing: Prior to initiation
Routine Monitoring
Clinical response (e.g., mood, neuropathic symptoms)
Frequency: Regularly, as clinically indicated (e.g., monthly for first few months, then quarterly)
Target: Improvement in symptoms
Action Threshold: Lack of improvement or worsening of symptoms may indicate need for dose adjustment or alternative therapy.
Homocysteine levels
Frequency: Every 3-6 months, if initially elevated and being treated.
Target: Normalization of levels (e.g., <15 mcmol/L)
Action Threshold: Persistent elevation may indicate inadequate dosing or other contributing factors.
Symptom Monitoring
- Improvement in depressive symptoms (e.g., mood, energy, anhedonia)
- Reduction in neuropathic pain or paresthesias
- Improved cognitive function
- Overall well-being
Special Patient Groups
Pregnancy
L-methylfolate (folate) is essential during pregnancy for proper fetal development, particularly for preventing neural tube defects. Supplementation is often recommended for all pregnant women. Category A.
Trimester-Specific Risks:
First Trimester:
Crucial for neural tube development; supplementation is highly recommended to reduce risk of defects.
Second Trimester:
Continued importance for fetal growth and development.
Third Trimester:
Continued importance for fetal growth and maternal health.
Lactation
L-methylfolate is compatible with breastfeeding. Folate is naturally present in breast milk and is essential for infant growth and development. Supplementation is generally considered safe and beneficial for both mother and infant.
Infant Risk:
Low risk (L1 - Safest)
Pediatric Use
While specific drug indications for L-methylfolate are not established in pediatric populations, folate supplementation is common and safe for children based on dietary needs or specific medical conditions (e.g., certain anemias, metabolic disorders). Dosing should be guided by a healthcare professional.
Geriatric Use
L-methylfolate is generally safe and well-tolerated in geriatric patients. It may be particularly beneficial for age-related cognitive decline, neuropathy, or in patients with MTHFR polymorphisms. No specific dose adjustments are typically required based on age alone.
Clinical Information
Clinical Pearls
- L-methylfolate is the active, bioavailable form of folate, bypassing the MTHFR enzyme step, which is beneficial for individuals with MTHFR polymorphisms.
- It is commonly used as an adjunctive therapy for major depressive disorder, especially in patients who have not responded adequately to antidepressants alone.
- Also utilized in the management of diabetic peripheral neuropathy and hyperhomocysteinemia.
- Generally very well-tolerated with a low side effect profile, making it a safe addition to many treatment regimens.
- Patients should be advised that it is a nutritional supplement/medical food and may not be covered by insurance like traditional prescription drugs.
Alternative Therapies
- For depression: other antidepressants, psychotherapy, ECT, TMS.
- For neuropathy: gabapentin, pregabalin, duloxetine, tricyclic antidepressants.
- For hyperhomocysteinemia: Vitamin B12, Vitamin B6.
Cost & Coverage
Average Cost:
Highly variable ($30 - $150+) per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Often not covered as a prescription drug by many insurance plans; may be covered as a medical food or through specific formularies. Patient may need to pay out-of-pocket.
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more details. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide information about the medication taken, the amount, and the time it happened.